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STAT3 inhibitor DG-4

Chemical Structure : STAT3 inhibitor DG-4

CAS No.:

STAT3 inhibitor DG-4

Catalog No.: PC-20605Not For Human Use, Lab Use Only.

DG-4 is a potent, selective inhibitor of STAT3-dependent transcription with IC50 of 0.12 uM in IL6-STAT3 luciferase reporter assays, 44-fold selectivity over IFN-γ STAT1.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DG-4 is a potent, selective inhibitor of STAT3-dependent transcription with IC50 of 0.12 uM in IL6-STAT3 luciferase reporter assays, 44-fold selectivity over IFN-γ STAT1.
DG-4 does not bind to cellular STAT3 but to another prominent anticancer drug target, TrxR1.
DG-4 inhibits TrxR1 activity and contribute to TrxR1 inhibitory effects in cells at 1 uM.
DG-4 induces oxidative stress leading to Prx2/STAT3 oxidation, subsequently blocks STAT3-dependent transcription and induces cell death.

Physicochemical Properties

M.Wt 395.28
Formula C18H20Cl2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NCCN1CCCCC1)C2=CC=C(N3C(C(Cl)=C(Cl)C=N3)=O)C=C2

References

1. S Busker, et al. Sci Adv. 2020 Mar 20;6(12):eaax7945.

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